Discovery of S-phase arresting agents derived from noscapine

被引:39
作者
Anderson, JT [1 ]
Ting, AE [1 ]
Boozer, S [1 ]
Brunden, KR [1 ]
Danzig, J [1 ]
Dent, T [1 ]
Harrington, JJ [1 ]
Murphy, SM [1 ]
Perry, R [1 ]
Raber, A [1 ]
Rundlett, SE [1 ]
Wang, JM [1 ]
Wang, N [1 ]
Bennani, YL [1 ]
机构
[1] Athersys Inc, Cleveland, OH 44115 USA
关键词
D O I
10.1021/jm0494220
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Analogues of the natural product noscapine were synthesized, and their potential as antitumor agents were examined. The discovery of a novel regio- and stereoselective O-demethylation led to the synthesis of several O-alkylated analogues that induced an unexpected S-phase arrest of mammalian cells. Compound 4a was the most potent analogue inhibiting cell proliferation at an EC50 of 1.9 mu M.
引用
收藏
页码:2756 / 2758
页数:3
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